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CX-4945 (Silmitasertib)

品牌 厂商性质 产地 货期
阿拉丁 生产商 上海 现货

询价
产品参数
货号 CAS号 操作
C127975-10mg 1009820-21-6 询价
C127975-50mg 1009820-21-6 询价
C127975-5mg 1009820-21-6 询价
产品介绍

  • 分子式 C19H12ClN3O2
  • 分子量349.77
  • Beilstein号
  • EC号
  • MDL号
  • PubChem编号

属性

溶解性 Soluble in water (<1.2 mg/ml), DMSO (≥65 mg/ml), and ethanol (<1.2 mg/ml).
存贮条件 储存温度-20°C

描述

应用 An ATP-competitive CK2 protein kinase inhibitor.
产品介绍 CX-4945 (Silmitasertib)是有效的,选择性CK2(casein kinase 2)抑制剂,无细胞试验中IC50为1 nM,对 Flt3, Pim1 和 CDK1作用效果稍弱(细胞试验中没有活性)。
备注 CX-4945 is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Phase 1.
生化机理 CX-4945 (Silmitasertib) is an ATP-competitive CK2 protein kinase inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively. CX-4945 has broad-spectrum anti-proliferative activity in multiple cancer cell lines. The anti-proliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. Attenuation of PI3K/Akt signaling by CX-4945 was evidenced by dephosphorylation of Akt on the CK2-specific S129 site and the canonical S473 and T308 regulatory sites. CX-4945 suppresses Akt signaling and inhibits proliferation of HUVEC Cells. CX-4945 causes cell-cycle arrest and selectively induced apoptosis in certain cancer cells. In models of angiogenesis, CX-4945 inhibited human umbilical vein endothelial cell migration, tube formation, and blocked CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells. Collectively, CX-4945 inhibits pro-angiogenic CK2 signaling in vitro and in vivo.
别名 CX-4945; CX 4945; CX4945; 5-[(3-氯苯基)氨基]苯并[c]-2,6-萘啶-8-羧酸;Silmitasertib;CX 4945;CX4945; 5-[(3-Chlorophenyl)amino]benzo[c]-2,6-naphthyridine-8-carboxylic acid

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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途